GSK239512 / GSK - LARVOL DELTA

Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta-Analysis. (PubMed, Neuropsychopharmacol Rep) - "Some H3R-ANTs/H3R-IAs might provide benefit for the treatment of cognitive symptoms and depressive symptoms in individuals afflicted with schizophrenia."

Clinical • Journal • Retrospective data • Review • CNS Disorders • Insomnia • Psychiatry • Schizophrenia • Sleep Disorder

Interventions promoting remyelination in multiple sclerosis: a systematic review of clinical trials. (PubMed, Neurol Res) - "Notably, rHIgM22, L-T3, opicinumab, clemastine fumarate, phenonytoin, domperidone, GSK239512, human fetal neural precursor cells (hfNPCs), and low-intensity repetitive transcranial magnetic stimulation (LI-rTMS) exhibited remyelination potential. Additionally, disease-modifying therapies (DMTs) such as Ocrelizumab, Fingolimod, and Natalizumab showed promising effects. Although several interventions demonstrated remyelination potential, limitations such as small sample sizes, short follow-up periods, and lack of standardized clinical endpoints validating remyelination's functional impact, highlight the need for robust clinical trial designs, advanced biomarkers, and combination therapies integrating remyelination, neuroprotection, and immunomodulation to improve MS treatment outcomes."

Journal • Review • CNS Disorders • Immunology • Inflammation • Multiple Sclerosis

Randomized, double-blind, placebo controlled, parallel group exploratory study of GSK239512 for cognitive impairment in stable schizophrenia subjects on background antipsychotic therapy (Society of Biological Psychiatry,67th Annual Meeting) - Presentation time: Thursday, May 03 2012, 5:00 PM - 6:30 PM; P2, N=50; NCT01009060; GSK239512 was well tolerated with mild improvement on CSSB total score; Effects on CSSB domains were positive or neutral, except processing speed, which favored PBO; Differences in MCCB were neutral or favored PBO except verbal learning

P2 data • Schizophrenia

Tau overexpression exacerbates neuropathology after repeated mild head impacts in male mice. (PubMed, Neurobiol Dis) - "Tau58.4 mice were treated with the histamine H3 receptor antagonist GSK239512 for 1-month post-injury to promote remyelination of white matter lesions...However, unlike immune-competent mice, R2G2 mice had altered myeloid cell gene expression and fewer demyelinated lesions. Together this data shows that rmTBI leads to chronic white matter inflammatory demyelination and axonal loss exacerbated by human tau overexpression but suggests that immune-suppression and remyelination alone are insufficient to reverse damage."

Journal

Approaches to Remyelination Therapies in Multiple Sclerosis. (PubMed, Curr Treat Options Neurol) - "Several recent clinical trials of remyelination therapies, including opicinumab, clemastine, and GSK239512, showed negative or modest results. To date, no therapies have led to robust remyelination. Future efforts to promote remyelination will likely require a combination of these mechanistic strategies."

Journal • Review